This invention relates to an improved formulation and process methodology of Coenzyme Q10 in producing soft gel capsules of this formulation. Coenzyme Q10 (CoQ10 or Ubiquinone) is a large molecular weight (863.63 grams) lipid compound that is produced in the liver and perhaps other body organs. The total body content is estimated to be 1.4 to 1.8 grams, depending on the age and the physical fitness of the individual. Although CoQ10 is found in the mitochondria and other organelles of every living cell, it appears to be most abundant in tissues with a high number of mitochondria and a high level of metabolic activity. For example, in the metabolically inactive blood there is approximately 4 mg, in the heart, and in the skeletal muscle 1000 mg. The blood acts as a CoQ10 reservoir and transport media between endogenous CoQ10 synthesis in the liver, exogenous CoQ10 absorption from digested food substances in the intestinal tract, and the body cells. Endogenous synthesis appears to be responsible for 56 percent and exogenous sources for 44 percent of the body""s CoQ10 requirements. These numbers are currently being studied and endogenous CoQ10 synthesis may be significantly deficient in the elderly. These deficiencies are not related to the total caloric intake, but rather to the vitamin content of ingested foods. The body requires multiple vitamins for the synthesis of CoQ10.
CoQ10 requirements of the body are also variable between individuals and are dependent on age, physical activity, and disease. It is estimated that the body CoQ10 utilization is between 5 and 9 mg per day. Intercellular CoQ10 is required for the synthesis of energy and therefore essential for life. Energy synthesis occurs in the mitochondria, where CoQ10 provides an electron for the electron transport chain in the cytochrome system, in which adenosine tripohosphate (ATP) is synthesized. As CoQ10 gives up an electron for ATP synthesis, it gets oxidized. If CoQ10 is used as an antioxidant, it gets oxidized and is no longer available to provide electrons and function in the synthesis of ATP. Under conditions of high metabolic stress, endogenous sources may become inadequate to meet the body""s CoQ10 requirement for ATP synthesis. Under such conditions, dietary CoQ10 supplementation has been shown to be an effective source. An improved soft gel formulation and process of CoQ10 soft gel capsule manufacturing has uses to treat heart failure, chronic fatigue and patients with psoriasis and planter warts. In all cases, it has been found that the improved soft gel formulation at ingestion rates of 30-100 mg/day of CoQ10 have been proven to be superior to commercially available 60 mg dry powder capsules, and existing 100 mg/day CoQ10 soft gel formulations.
An appropriate CoQ10 dosage for a normal individual compared to the dosage necessary for a diseased individual has been difficult to ascertain. Recommended doses of 10 to 30 mg/day were found to be ineffective for patients with significant CoQ10 deficiencies. In the past 15 years, it has become generally accepted that poor intestinal absorption of certain CoQ10 formulations limits their effective use. For this reason, 50 and 150 mg CoQ10 containing tablets or capsules are commercially available to the consumer, at a considerably higher cost.
Folkers et al (U.S. Pat. No. 4,824,669) addresses a soft gel capsule with CoQ10 and at least one vegetable oil. This formulation was determined to increase blood CoQ10 levels to 2.5 xcexcg/ml compared to 1.6 xcexcg/ml for an equivalent 100 mg dose of dry powder CoQ10. Many different CoQ10 formulations have appeared which are claimed to increase intestinal absorption. However, intestinal absorption data, collected under near basal conditions, which compare CoQ10 alone in oil with dry powder CoQ10, are conclusive that oil is a better delivery agent.
The present invention comprises a stable and nontoxic soft gel Coenzyme Q10 formulation and process methodology of Coenzyme Q10 for maximum Coenzyme Q10 levels in the human body for a given input. A preferred soft gel formulation includes Coenzyme Q10 (hereinafter CoQ10), Vitamin E, beta-carotene, bee""s wax, medium chain triglycerides available as MCT Myglyol S12, and rice bran oil formulated to maximize the body""s absorption by maintaining the CoQ10 in what may be a supersaturated solution in easily absorbed materials, that can provide healthful effects, as opposed to just fillers. It is important as much of the supplied CoQ10 be absorbed, rather than just taking megadoses at frequent intervals as the wholesale cost of CoQ10 dry powder in quantity is as much as $2000 per kg. Not only is a relatively large percentage of the CoQ10 absorbed, but the volume of the soft gel capsule is minimized, making it easier to swallow and requiring smaller shipping and storage space. Recent studies indicate the preferred soft gel CoQ10 formulation should be administered twice a day in dosages of about 30 mg CoQ10 in 220 mg capsules, as that amount of CoQ10 is about the maximum the body of a healthy sedentary adult can use for maintenance of a preferred blood level. For those who have deficiencies of CoQ10, studies have shown that twice a day administration of about 60 mg CoQ10 in 435 mg capsules is advantageous. In special instances of CoQ10 deficiency, twice a day ingestion of 100 mg CoQ10 containing soft gel capsules can be tolerated.
It is therefore an object of the present invention to provide a soft gel formulation of CoQ10 and a methodology of formulation processing that produce a significantly greater bioavailability percentage of ingested CoQ10 than existing soft or dry formulations.
Another object of the present invention is to provide a soft gel formulation of CoQ10 and methodology of administration that produces greater absorption of CoQ10 into the intestine.
Another object is to minimize the ingested volume required to maintain a given CoQ10 blood content.
Another object is to provide a process that keeps CoQ10 in solution in readily absorbed materials, that themselves have beneficial effects.